ArticleNature communications2021
Checkpoint inhibition through small molecule-induced internalization of programmed death-ligand 1.
Article in Nature communications, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 65 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
65 citing papers in PubMed, 131 citations in OpenAlex.
- Exploring FDA-approved small molecules for their potential as PD-1/PD-L1 inhibitors: integrating computational screening with experimental testing.Journal of molecular modeling · 2026Article
- Small molecules targeting the PD-1/PD-L1 axis for cancer immunotherapy.Theranostics · 2026Review
- Dual-targeting CD73/PD-L1 bifunctional inhibitor: a promising cancer immunotherapy strategy.Frontiers in immunology · 2026Article
- Synthesis and Anti-Tumor Evaluation of Carboranyl BMS-202 Analogues-A Case of Carborane Not as Phenyl Ring Mimetic.Molecules (Basel, Switzerland) · 2025Article
- Computational identification and evaluation of novel PD-L1 inhibitors for cancer immunotherapy.Scientific reports · 2025Article
- Characterization of Clinically Evaluated Small-Molecule Inhibitors of PD-L1 for Immunotherapy.ACS medicinal chemistry letters · 2025Article
- Ex vivo engineering of phagocytic signals in breast cancer cells for a whole tumor cell-based vaccine.BMC cancer · 2025Article
- Immune checkpoint inhibitors in cancer therapy: what lies beyond monoclonal antibodies?Medical oncology (Northwood, London, England) · 2025Review
- Review
- Negative Immune Checkpoint Inhibitors.Pharmaceutics · 2025Review
- Advancements in drug discovery: integrating CADD tools and drug repurposing for PD-1/PD-L1 axis inhibition.RSC advances · 2025Article
- Article
- Advancing Cancer Immunotherapy through Engineering New PD-L1 Degraders: A Comprehensive Study from Small Molecules to PD-L1-Specific Peptide-Drug Conjugates.Journal of medicinal chemistry · 2024Article
- Molecular insight into binding affinities and blockade effects of selected flavonoid compounds on the PD-1/PD-L1 pathway.RSC advances · 2024Article
- Miniprotein engineering for inhibition of PD-1/PD-L1 interaction.Protein science : a publication of the Protein Society · 2024Article
- Nonsymmetrically Substituted 1,1'-Biphenyl-Based Small Molecule Inhibitors of the PD-1/PD-L1 Interaction.ACS medicinal chemistry letters · 2024Article
- C2-Symmetrical Terphenyl Derivatives as Small Molecule Inhibitors of Programmed Cell Death 1/Programmed Death Ligand 1 Protein-Protein Interaction.Molecules (Basel, Switzerland) · 2024Article
- In Search of Better Peptide-(Derived from PD-L2)-Based Immune Checkpoint Inhibitors.Biomolecules · 2024Article
- Multiparatopic antibodies induce targeted downregulation of programmed death-ligand 1.Cell chemical biology · 2024Article
- Development of small molecule drugs targeting immune checkpoints.Cancer biology & medicine · 2024Review
5 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
23 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Programmed death-ligand 1 is a glycoprotein expressed on antigen presenting cells, hepatocytes, and tumors which upon interaction with programmed death-1, results in inhibition of antigen-specific T cell responses. Here, we report a mechanism of inhibiting programmed death-ligand 1 through small molecule-induced dimerization and internalization. This represents a mechanism of checkpoint inhibition, which differentiates from anti-programmed death-ligand 1 antibodies which function through molecular disruption of the programmed death 1 interaction. Testing of programmed death ligand 1 small molecule inhibition in a humanized mouse model of colorectal cancer results in a significant reduction in tumor size and promotes T cell proliferation. In addition, antigen-specific T and B cell responses from patients with chronic hepatitis B infection are significantly elevated upon programmed death ligand 1 small molecule inhibitor treatment. Taken together, these data identify a mechanism of small molecule-induced programmed death ligand 1 internalization with potential therapeutic implications in oncology and chronic viral infections.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.